Use of combined nanocarrier system based on chitosan nanoparticles and phospholipids complex for improved delivery of ferulic acid

Telange, Darshan R.; Jain, Shirish P.; Pethe, Anil M.; Kharkar, Prashant S.; Rarokar, Nilesh R.

doi:10.1016/j.ijbiomac.2020.12.211

Cited by 22 publications

(8 citation statements)

References 62 publications

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“…The DSC scanned images were read and interpreted using instrument-attached software (UA, V4.5A, build 4.5.0.5). The method reported by our group earlier was used for the DSC analysis (Telange et al., 2021a ).…”

Section: Methodsmentioning

confidence: 99%

Development of phospholipon®90H complex nanocarrier with enhanced oral bioavailability and anti-inflammatory potential of genistein

Shete

Telange

Mahajan³

et al. 2023

Drug Delivery

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Genistein (GEN), an isoflavonoid, offers multifunctional biological activities. However, its poor oral bioavailability, aqueous solubility, extensive metabolism, and short half-life restricted its clinical use. Therefore, the Phospholipon ® 90H complex of genistein (GPLC) was prepared to enhance its biopharmaceutical properties and anti-inflammatory activity. GPLC was characterized by employing particle size and zeta potential, Fourier transforms infrared spectrophotometry, differential scanning calorimetry, powder x-ray diffractometry, proton nuclear magnetic resonance, aqueous solubility, in vitro dissolution, ex vivo permeation, oral bioavailability and in vivo anti-inflammatory activity. The complex showed high entrapment of GEN (∼97.88% w/w) within the Phospholipon ® 90H matrix. Particle size and zeta potential studies confirmed the small particle size with the modest stability of GPLC. The characterization analysis supported the formation of GPLC through the participation of hydrogen bonding between GEN and Phospholipon ® 90H. GPLC significantly enhanced the aqueous solubility (∼2-fold) compared to GEN. Dissolution studies revealed that GPLC drastically improved the GEN dissolution rate compared to GEN. Likewise, the complex improved the permeation rate across the membrane compared to GEN. GPLC formulation significantly enhanced the oral bioavailability of GEN via improving its Cmax, tmax, AUC, half-life and mean residence time within the blood circulation compared to GEN. The GPLC (∼20 mg/kg, p.o.) remarkably inhibited the increase in paw edema up to 5 h, compared to GEN and diclofenac. Results suggest that the Phospholipon ® 90 complex is a superior and promising carrier for enhancing the biopharmaceutical parameters of GEN and other bioactive with similar properties.

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Section: Methodsmentioning

confidence: 99%

Development of phospholipon®90H complex nanocarrier with enhanced oral bioavailability and anti-inflammatory potential of genistein

Shete

Telange

Mahajan³

et al. 2023

Drug Delivery

Self Cite

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“…An excellent way to increase the delivery of FA after oral administration was the development of a new nanocarrier system based on chitosan nanoparticles loaded with phospholipid complex (FAPLC CNP) [ 86 ]. Another method to improve therapeutic efficacy of ferulic acid may be using aerosolized chitosan nanoparticles, which are supposed to be effective in treatment of asthma [ 87 ].…”

Section: Novel Strategies For Ferulic Acid Drug Deliverymentioning

confidence: 99%

Recent Advances in Biological Activity, New Formulations and Prodrugs of Ferulic Acid

Stompor-Gorący

Machaczka

2021

IJMS

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Trans-ferulic acid (FA) is a derivative of 4-hydroxycinnamic acid, which is found in many food products, fruits and beverages. It has scientifically proven antioxidant, anti-inflammatory and antibacterial properties. However, its low ability to permeate through biological barriers (e.g., the blood–brain barrier, BBB), its low bioavailability and its fast elimination from the gastrointestinal tract after oral administration limit its clinical use, e.g., for the treatment of neurodegenerative diseases, such as Alzheimer’s disease. Therefore, new nanotechnological approaches are developed in order to regulate intracellular transport of ferulic acid. The objective of this review is to summarize the last decade’s research on biological properties of ferulic acid and innovative ways of its delivery, supporting pharmacological therapy.

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“…Nevertheless, its clinical application in the pharmaceutical field is still limited due to its low oral bioavailability, fast metabolism, and elimination after oral administration [179]. In one study, Telange et al developed FA-phospholipid complex-loaded CS-NPs (FA-PLC-CS-NPs) for improved oral bioavailability in Wistar rats [180]. The developed FA-PLC-CS-NPs exhibited almost 2-fold higher intestinal permeation compared to the free drug solution.…”

Section: Ferulic Acidmentioning

confidence: 99%

Recent Advancement in Chitosan-Based Nanoparticles for Improved Oral Bioavailability and Bioactivity of Phytochemicals: Challenges and Perspectives

et al. 2021

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The excellent therapeutic potential of a variety of phytochemicals in different diseases has been proven by extensive studies throughout history. However, most phytochemicals are characterized by a high molecular weight, poor aqueous solubility, limited gastrointestinal permeability, extensive pre-systemic metabolism, and poor stability in the harsh gastrointestinal milieu. Therefore, loading of these phytochemicals in biodegradable and biocompatible nanoparticles (NPs) might be an effective approach to improve their bioactivity. Different nanocarrier systems have been developed in recent decades to deliver phytochemicals. Among them, NPs based on chitosan (CS) (CS-NPs), a mucoadhesive, non-toxic, and biodegradable polysaccharide, are considered the best nanoplatform for the oral delivery of phytochemicals. This review highlights the oral delivery of natural products, i.e., phytochemicals, encapsulated in NPs prepared from a natural polymer, i.e., CS, for improved bioavailability and bioactivity. The unique properties of CS for oral delivery such as its mucoadhesiveness, non-toxicity, excellent stability in the harsh environment of the GIT, good solubility in slightly acidic and alkaline conditions, and ability to enhance intestinal permeability are discussed first, and then the outcomes of various phytochemical-loaded CS-NPs after oral administration are discussed in detail. Furthermore, different challenges associated with the oral delivery of phytochemicals with CS-NPs and future directions are also discussed.

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Use of combined nanocarrier system based on chitosan nanoparticles and phospholipids complex for improved delivery of ferulic acid

Cited by 22 publications

References 62 publications

Development of phospholipon®90H complex nanocarrier with enhanced oral bioavailability and anti-inflammatory potential of genistein

Development of phospholipon®90H complex nanocarrier with enhanced oral bioavailability and anti-inflammatory potential of genistein

Recent Advances in Biological Activity, New Formulations and Prodrugs of Ferulic Acid

Recent Advancement in Chitosan-Based Nanoparticles for Improved Oral Bioavailability and Bioactivity of Phytochemicals: Challenges and Perspectives

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